中文名称: A438079
英文名称: A438079
CAS No: 899507-36-9
分子式: C13H9Cl2N5
分子量: 306.15
A12328 A438079 ≥98% (psaitong)
包装规格:
10mg 50mg 100mg in glass bottle
溶解性:
溶于DMSO(100mg/ml超声)
产品描述:

基本信息

产品编号:

A12328

产品名称:

A438079

CAS:

899507-36-9

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C13H9Cl2N5

溶于液体

-80℃

6个月

分子量:

306.15

-20℃

1个月

化学名: 

A438079 3-((5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl)methyl)pyridine

Solubility (25°C):

 

体外:

 

DMSO

 

Ethanol

 

Water

 

体内(现配现用):

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

3.2664mL

16.3319mL

32.6637mL

5mM

0.6533mL

3.2664mL

6.5327mL

10mM

0.3266mL

1.6332mL

3.2664mL

 

生物活性

产品描述

一种有效的,选择性的P2X7受体拮抗剂,pIC50值为6.9。

靶点

pIC50:6.9 (P2X7 receptor)

 

体外研究

In 1321N1 cells stably expressing rat P2X7 receptors,A 438079 blocks BzATP-(10μM) evoked changes in intracellular calcium concentrations with an IC50 of 321nM.A 438079 is also selective for the P2X7 receptor,at concentrations up to 100μM.

体内研究

A 438079 (80μmol/kg,i.v.) reduces noxious and innocuous evoked activity of different classes of spinal neurons in neuropathic rats.A 438079 (100 and 300μmol/kg,i.p.) significantly raises withdrawal thresh-olds in both the SNL and CCI models.Intraperitoneal injection of A 438079 (5 and 15mg/kg) 60 min after triggering seizures reduces seizure severity and neuronal death within the hippocampus.A 438079 has superior neuroprotective effects compared with an equally dose of phenobarbital (25mg/kg).A 438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores.Pretreatment with A 438079 reduces nociceptive behaviour scores in the HC model.

 

推荐实验方法(仅供参考)

激酶实验:

Human astrocytoma cells,1321N1,are grown to stably express rat P2X7,human P2X4,P2X2a, P2X2/3,P2X1,P2Y1 and P2Y2 recombinant receptors.Agonist,BzATP,2,3-O-(4-ben-zoylbenzoyl)-ATP or ATP-induced changes in intracellular Ca2+ concentrations are assessed in all of the cell lines using the Ca2+ chelating dye,Fluo-4,in conjunction with a Fluorometric Imaging Plate Reader.The cells are plated out the day before the experiment onto poly-D-lysine-coated black 96 well plates.After the agonist addition, changes in intracellular Ca2+ concentrations are recorded,per second,for 3 min.Ligands are tested at 11 half-log concentrations from 10-10 to 10-4M.BzATP or ATP concentrations corresponds to the EC70 values for each receptor to enable comparison of antagonist potencies across the multiple P2 receptor subtypes.A 438079 is added to the cell plate and fluorescence data are collected for 3 min before the addition of agonist,subsequently,data are then collected for another 2 min.The pEC50 or pIC50 values are derived from a single curve fit.

 

动物实验:

 

To confirm A 438079 reach the brain after systemic administration,P10 rat pups are injected with 5mg/kg A 438079 and killed either 10 min,30 min,or 2h later (n=4 per group).Blood samples are centrifuged at 1000×g for 10 min to isolate the plasma.Samples are analyzed using liquid chromatography-mass spectrometry (LC-MS/MS) by a service provider.Briefly,protein is precipitated from 50μL aliquots of the individual plasma or brain tissue homogenate,and A 438079 is quantified by LC-MS/MS from a five-point standard curve.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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